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Tablets and some equations for determination of forces affecting tablet compaction

Year 2015, Volume: 5 Issue: 3, 204 - 210, 01.10.2015

Abstract

Tablet is the most common pharmaceutical dosage form in drug industry. It is classified as a solid dosage form. Due to its advantage, it is widely produced and used. Excipient type and level are very important for tablet formulation. Presence of a lubricant in a tablet formulation is necessary for production. Lubricants determine the specification of the final product and improve tablet performance. Lubricants also show glidant effects. During tablet production, the frictional forces between the compression machine components must be reduced with the use of an ideal lubricant. By adding a lubricant to the formulation, a layer is built around each powder particle which causes lesser tablet deformation. The effect of the lubricants on tablet’s mechanical property is related to their binding mechanism. The principle of tablet press instrumentation is to measure the forces on the dies and those transferred from the dies to other components of the press. Lubricant activity of the excipients can be evaluated using the formulated data that include tensile strength, cohesion index, lubricant effectiveness and transmission ratio.

References

  • Bauer KH, Frömming KH, Führer C. (2012). Pharmazeutische Technologie Mit Einführung in die Biopharmazie. 9. Auflage, Wissenschaftliche Verlagsgesellschaft, Stuttgart. 2012, p.600-644.
  • Rawlins EA. Bentley’s Textbook of Pharmaceutics. 8th edition, Part II, Bailliere Tindall, London. 1982. p. 263-319.
  • King ER. Tablets, Capsules and Pills. In: Remington’s Pharmaceutical Sciences. Ed: Hoover JE, 15th Edition, Mack Publishing Company, Pennsylvania. 1975. p.595-625.
  • Shotton E, Ridgway K. Physical Pharmaceutics. In: Pharmaceutical Preperations, Clarendon Press, Oxford. 1974. p.264-273.
  • Marshall K, Rudnic EM. Tablet Dosage Forms. In: Modern Pharmaceutics Eds: Banker GS, Rhodes CT, second ed, Marcel Dekker Inc, New York USA. 1990. p.88-127.
  • Kumar V, Reus-Medina MDIL, Yang D. Preparation, characterization, and tabletting properties of a new cellulose-based pharmaceutical aid. Int J Pharm. 2002;235(1-2):129-140.
  • Müller FS. Modified celluloses as multifunctional excipients in rapidly dissolving immediate release tablets. University of Basel, Faculty of Science. PhD Thesis, Switzerland. 2008.
  • Jain S. Mechanical Properties of Powders for Compaction and Tableting: An Overview. Pharm Sci Technol Today. 2008;2 (1):20-31.
  • Nyström C, Karehill, PG. The Importance of Intermoleculer Bonding Forces and the Concept of Bonding Surface Area. In: Pharmaceutical Powder Compaction Technology Vol. 71 Ed: Nyström C. Marcel Dekker Inc. 1995.p.1-55.
  • Auton EM. Parmaceutics: The Science Of Dosage Form Designs, New York, U.S.A. 1988. p. 304-321.
  • Patel SS, Patel NM. Development of directly compressible co-processed excipient for dispersible tablets using 32 full factorial desing. Int J Pharm Pharm Sci. 2009;1(1):125-148.
  • Sheth BB, Bandelin FJ, Shangraw RF. Compressed Tablets. In: Pharmaceutical Dosage Forms Vol.1 “Tablets” Ed: Lieberman HA, Lachman L. Marcel Dekker Inc. New York, USA. 1980.p.109-184.
  • Yuan J, Wu SHW. Sustained release tablets via direct compression: A feasibility study using cellulose acetate and cellulose acetate butyrate. Pharm Dev Technol. 2008;24:92-106.
  • Gohel MC. A review of co-processed directly compressible excipients. J Pharm Sci. 2003;8:76-93.
  • Zhang Y, Law Y, Chakrabarti S. Physical properties and compact analysis of commonly used direct compression binders. AAPS Pharm Sci Tech. 2003;4(4):1-11.
  • Pontier C, Champion E, Viana M, Chulia D, Assollant DB. Use of cycles of compression to characterize the behavior of apatitic phosphate powders. J Eur Ceram Soc. 2002;22:1205-1216.
  • Geçgil Ş. Farmasötik Teknolojiye Başlangıç. Cihan Matbaacılık, İstanbul. 1991. p.340-351.
  • Esposito P, Oobetti L, Boltri L, Rabaglia L. Use of novel neutron activable excipient “samarium stearate” as lubricant in tablets. Eur J Pharm Biopharm. 1994;40(5):341-343.
  • Şahin İ. Enstrümantal Tablet Presinde Lubrikant Performansının Değerlendirilmesi. M.Ü. Sağlık Bilimleri Enstitüsü, Yüksek Lisans Tezi, İstanbul, 2003.
  • Shah AC, Mlodozeniec AR. Mechanism of surface lubrication: Influence of duration of lubricant-excipient mixing on processing characteristics of powders and properties of compressed tablets. J Pharm Sci. 1977;66(10):1377-1382.
  • Gold G, Palermo BT. Hopper flow electrostatics of tabletting material II: tablet lubricants. J Pharm Sci. 1965;54(10):1571-1519.
  • York P. Application of powder failure testing equipment in assesing effect of glidants on flowability of cohesive pharmaceutical powders. J Pharm Sci. 1975;64(7):1216-1221.
  • Shah NH, Stiel D, Weiss M, Infeld MH, Malick AW. Evaluation of two new tablet lubricants-sodium stearyl fumarate and glyceryl behenate, measurements of physical parameters “compaction, ejection and residual forces” in the tabletting and the effect on the dissolution rate. Drug Dev Ind Pharm. 1986;12(8-9):1329-1346.
  • Bolhuis GK, Hölzer AW. Lubricant Sensivity. In: Pharmaceutical Powder Compaction Technology. Ed: Alderbom G, Marcel Dekker Inc, New York, USA, 1996.p.419-558.
  • Kikuta JI, Kitamori N. Effect of mixing time on the lubricating properties of magnesium stearate and the final characteristics of the compressed tablets. Drug Dev Ind Pharm. 1994;20(3):343-355.
  • Hwang R, Parrott EL. Effect of a lubricant on wear rate of tablets. Drug Dev lnd Pharm. 1993;19(12):1379-1391.
  • Aoshima H, Miyagisnima A, Nozawa Y, Saduka Y, Sonobe T. Glycerin fatty acid esters as a new lubricant of tablets. Int J Pharm. 2005;293:25-34.
  • Takeuchi H, Nagira S, Aikawa H, Yamamoto H, Kawashima Y. Effect of lubrication on the compaction properties of pharmaceutical excipients as measured by die wall pressure. J Drug Dev Sci Technol. 2005;15(2):177-182.
  • Alderborn G, Wikberg M. Granule Properties. In: Pharmaceutical Powder Compaction Technology. Eds: Alderborn G, Nyström C, Marcel Dekker, Inc, New York, USA, 1998.p.323-327.
  • Badawy SI, Williams RC, Gilbert DC. Effect of different acids on solid state stability of an ester prodrug of a IIb/IIIa glycoprotein receptor antagonist. Pharm Dev Technol. 1999;4(3):325-331.
  • Kikuta JI, Kitamori N. Effect of mixing time on the lubricating properties of magnesium stearate and the final characteristics of the compressed tablets. Drug Dev Ind Pharm.1994; 20(3):343-355.
  • Davies MC, Brown A, Newton JM. Chemical characterisation of lubricant films. J Pharm Pharmacol. 1987;39:122-124.
  • Delacourte A, Guyot JC. Efficacy and lubrication mechanism in tablet technology, Pharmaceutical Technology. In: Tabletting Technology. Eds: Rubinstein MH, Wells JI, Vol 2 “Compression”, Ellis Horwood Limited, New York. 1987.p.80-90.
  • Jones TM. The physicotechnical properties of starting materials used in tablet formulation. Int J Pharm Prod Manuf. 1981;2:17-24.
  • Fell JT, Newton JM, Determination of tablet strength by the diametrical compression test. J Pharm Sci. 1970;59:688-691.
  • Davies PN, Worthington HEC, Podczeck F, Newton JM. The determination of the mechanical strength of tablets of different shapes. Int J Pharm. 2003;258:153-163.
  • Ugurlu T, Halacoglu MD. Effects of some lubricants and evaluation of compression parameters on directly compressible powders. Pharm Dev Techol. 2014;19(3):347-354
  • Delacourte A, Predella P, Leterme P, Provasi D, Colombo P, Conte U, Catellani PL, Guyot JC. A method for quantitative evaluation of the effectiveness of the lubricants used in tablet tecnology. Drug Dev Ind Pharm. 1993;19(9):1047-1060.
  • Röscheisen G, Schmidt PC. The combination of factorial design and simplex method in the optimization of lubricants for effervescent tablets. Eur J Pharm Biopharm. 1995;41:302-308.
  • Mollan MJ, Celik M. The effects of lubrication on the compaction and post compaction properties of directly compressible maltodextrins. Int J Pharm. 1996;144(128):1-9.
  • Turkoglu M, Sahin I, San T. Evaluation of hexagonal boron nitride as a new tablet lubricant. Pharm Dev Technol. 2005;10:381-388.
  • Ugurlu T, Turkoglu M. Hexagonal boron nitride as a tablet lubricant and a comparison with conventional lubricants. Int J Pharm. 2008;353:45-51.
  • Turkoglu M, Ugurlu T, Halacoglu MD. Effects of lubricants on binary direct compression mixtures. Drug Discov Ther. 2010;4(2):123-128.

Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler

Year 2015, Volume: 5 Issue: 3, 204 - 210, 01.10.2015

Abstract

Tabletler ilaç endüstrisinde en çok kullanılan farmasötik dozaj şekilleridir. Katı dozaj şekilleri sınıfına girerler. Yaygın olarak üretilmesi ve kullanılması avantajlarından dolayıdır. Uygun bir yardımcı madde ve bu yardımcı maddelerin formülasyon içindeki seviyelerinin seçimi başarılı bir üretim için çok önemlidir. Tablet formülasyonu için gerekli olan yardımcı madde sınıflarından biri ise kaydırıcılardır. Son ürünün spesifikasyonlarının belirlenmesi ve basım performansının iyileştirmesi nedeniyle oldukça önemli yardımcı maddelerdir. Kaydırıcılar lubrikant ve glidant özelliklerde olmalıdır. İdeal bir kaydırıcı toz ve tablet basım makinasının tüm aksamları arasındaki sürtünme kuvvetini azaltma yeteneğine sahip olmalıdır. Kaydırıcılar, formülasyona ilave edildiklerinde, toz partikülleri etrafında tabaka oluşturmaktadır. Bu tabaka tabletlerin daha az deformasyona uğramasına neden olmaktadır. Lubrikantların tabletin mekanik özellikleri üzerine etkisi bağlanma mekanizması ile yakından ilgilidir. Tablet basım kuvvetini ölçmek amacıyla tablet presleri, zımba üzerinde oluşan kuvvetin, tablet presinin diğer aksamlarına aktarılması prensibi göz önünde bulundurularak enstrümante edilirler. Tablet basım makinası enstrümantasyonu sonrasında gerilme kuvveti, kohezyon indeksi, lubrikant etkinliği ve iletim oranı gibi verilerle lubrikant etkinliği değerlendirilir.

References

  • Bauer KH, Frömming KH, Führer C. (2012). Pharmazeutische Technologie Mit Einführung in die Biopharmazie. 9. Auflage, Wissenschaftliche Verlagsgesellschaft, Stuttgart. 2012, p.600-644.
  • Rawlins EA. Bentley’s Textbook of Pharmaceutics. 8th edition, Part II, Bailliere Tindall, London. 1982. p. 263-319.
  • King ER. Tablets, Capsules and Pills. In: Remington’s Pharmaceutical Sciences. Ed: Hoover JE, 15th Edition, Mack Publishing Company, Pennsylvania. 1975. p.595-625.
  • Shotton E, Ridgway K. Physical Pharmaceutics. In: Pharmaceutical Preperations, Clarendon Press, Oxford. 1974. p.264-273.
  • Marshall K, Rudnic EM. Tablet Dosage Forms. In: Modern Pharmaceutics Eds: Banker GS, Rhodes CT, second ed, Marcel Dekker Inc, New York USA. 1990. p.88-127.
  • Kumar V, Reus-Medina MDIL, Yang D. Preparation, characterization, and tabletting properties of a new cellulose-based pharmaceutical aid. Int J Pharm. 2002;235(1-2):129-140.
  • Müller FS. Modified celluloses as multifunctional excipients in rapidly dissolving immediate release tablets. University of Basel, Faculty of Science. PhD Thesis, Switzerland. 2008.
  • Jain S. Mechanical Properties of Powders for Compaction and Tableting: An Overview. Pharm Sci Technol Today. 2008;2 (1):20-31.
  • Nyström C, Karehill, PG. The Importance of Intermoleculer Bonding Forces and the Concept of Bonding Surface Area. In: Pharmaceutical Powder Compaction Technology Vol. 71 Ed: Nyström C. Marcel Dekker Inc. 1995.p.1-55.
  • Auton EM. Parmaceutics: The Science Of Dosage Form Designs, New York, U.S.A. 1988. p. 304-321.
  • Patel SS, Patel NM. Development of directly compressible co-processed excipient for dispersible tablets using 32 full factorial desing. Int J Pharm Pharm Sci. 2009;1(1):125-148.
  • Sheth BB, Bandelin FJ, Shangraw RF. Compressed Tablets. In: Pharmaceutical Dosage Forms Vol.1 “Tablets” Ed: Lieberman HA, Lachman L. Marcel Dekker Inc. New York, USA. 1980.p.109-184.
  • Yuan J, Wu SHW. Sustained release tablets via direct compression: A feasibility study using cellulose acetate and cellulose acetate butyrate. Pharm Dev Technol. 2008;24:92-106.
  • Gohel MC. A review of co-processed directly compressible excipients. J Pharm Sci. 2003;8:76-93.
  • Zhang Y, Law Y, Chakrabarti S. Physical properties and compact analysis of commonly used direct compression binders. AAPS Pharm Sci Tech. 2003;4(4):1-11.
  • Pontier C, Champion E, Viana M, Chulia D, Assollant DB. Use of cycles of compression to characterize the behavior of apatitic phosphate powders. J Eur Ceram Soc. 2002;22:1205-1216.
  • Geçgil Ş. Farmasötik Teknolojiye Başlangıç. Cihan Matbaacılık, İstanbul. 1991. p.340-351.
  • Esposito P, Oobetti L, Boltri L, Rabaglia L. Use of novel neutron activable excipient “samarium stearate” as lubricant in tablets. Eur J Pharm Biopharm. 1994;40(5):341-343.
  • Şahin İ. Enstrümantal Tablet Presinde Lubrikant Performansının Değerlendirilmesi. M.Ü. Sağlık Bilimleri Enstitüsü, Yüksek Lisans Tezi, İstanbul, 2003.
  • Shah AC, Mlodozeniec AR. Mechanism of surface lubrication: Influence of duration of lubricant-excipient mixing on processing characteristics of powders and properties of compressed tablets. J Pharm Sci. 1977;66(10):1377-1382.
  • Gold G, Palermo BT. Hopper flow electrostatics of tabletting material II: tablet lubricants. J Pharm Sci. 1965;54(10):1571-1519.
  • York P. Application of powder failure testing equipment in assesing effect of glidants on flowability of cohesive pharmaceutical powders. J Pharm Sci. 1975;64(7):1216-1221.
  • Shah NH, Stiel D, Weiss M, Infeld MH, Malick AW. Evaluation of two new tablet lubricants-sodium stearyl fumarate and glyceryl behenate, measurements of physical parameters “compaction, ejection and residual forces” in the tabletting and the effect on the dissolution rate. Drug Dev Ind Pharm. 1986;12(8-9):1329-1346.
  • Bolhuis GK, Hölzer AW. Lubricant Sensivity. In: Pharmaceutical Powder Compaction Technology. Ed: Alderbom G, Marcel Dekker Inc, New York, USA, 1996.p.419-558.
  • Kikuta JI, Kitamori N. Effect of mixing time on the lubricating properties of magnesium stearate and the final characteristics of the compressed tablets. Drug Dev Ind Pharm. 1994;20(3):343-355.
  • Hwang R, Parrott EL. Effect of a lubricant on wear rate of tablets. Drug Dev lnd Pharm. 1993;19(12):1379-1391.
  • Aoshima H, Miyagisnima A, Nozawa Y, Saduka Y, Sonobe T. Glycerin fatty acid esters as a new lubricant of tablets. Int J Pharm. 2005;293:25-34.
  • Takeuchi H, Nagira S, Aikawa H, Yamamoto H, Kawashima Y. Effect of lubrication on the compaction properties of pharmaceutical excipients as measured by die wall pressure. J Drug Dev Sci Technol. 2005;15(2):177-182.
  • Alderborn G, Wikberg M. Granule Properties. In: Pharmaceutical Powder Compaction Technology. Eds: Alderborn G, Nyström C, Marcel Dekker, Inc, New York, USA, 1998.p.323-327.
  • Badawy SI, Williams RC, Gilbert DC. Effect of different acids on solid state stability of an ester prodrug of a IIb/IIIa glycoprotein receptor antagonist. Pharm Dev Technol. 1999;4(3):325-331.
  • Kikuta JI, Kitamori N. Effect of mixing time on the lubricating properties of magnesium stearate and the final characteristics of the compressed tablets. Drug Dev Ind Pharm.1994; 20(3):343-355.
  • Davies MC, Brown A, Newton JM. Chemical characterisation of lubricant films. J Pharm Pharmacol. 1987;39:122-124.
  • Delacourte A, Guyot JC. Efficacy and lubrication mechanism in tablet technology, Pharmaceutical Technology. In: Tabletting Technology. Eds: Rubinstein MH, Wells JI, Vol 2 “Compression”, Ellis Horwood Limited, New York. 1987.p.80-90.
  • Jones TM. The physicotechnical properties of starting materials used in tablet formulation. Int J Pharm Prod Manuf. 1981;2:17-24.
  • Fell JT, Newton JM, Determination of tablet strength by the diametrical compression test. J Pharm Sci. 1970;59:688-691.
  • Davies PN, Worthington HEC, Podczeck F, Newton JM. The determination of the mechanical strength of tablets of different shapes. Int J Pharm. 2003;258:153-163.
  • Ugurlu T, Halacoglu MD. Effects of some lubricants and evaluation of compression parameters on directly compressible powders. Pharm Dev Techol. 2014;19(3):347-354
  • Delacourte A, Predella P, Leterme P, Provasi D, Colombo P, Conte U, Catellani PL, Guyot JC. A method for quantitative evaluation of the effectiveness of the lubricants used in tablet tecnology. Drug Dev Ind Pharm. 1993;19(9):1047-1060.
  • Röscheisen G, Schmidt PC. The combination of factorial design and simplex method in the optimization of lubricants for effervescent tablets. Eur J Pharm Biopharm. 1995;41:302-308.
  • Mollan MJ, Celik M. The effects of lubrication on the compaction and post compaction properties of directly compressible maltodextrins. Int J Pharm. 1996;144(128):1-9.
  • Turkoglu M, Sahin I, San T. Evaluation of hexagonal boron nitride as a new tablet lubricant. Pharm Dev Technol. 2005;10:381-388.
  • Ugurlu T, Turkoglu M. Hexagonal boron nitride as a tablet lubricant and a comparison with conventional lubricants. Int J Pharm. 2008;353:45-51.
  • Turkoglu M, Ugurlu T, Halacoglu MD. Effects of lubricants on binary direct compression mixtures. Drug Discov Ther. 2010;4(2):123-128.
There are 43 citations in total.

Details

Primary Language Turkish
Journal Section Articles
Authors

Mekin Doğa Halaçoğlu This is me

Timuçin Uğurlu

Publication Date October 1, 2015
Submission Date October 1, 2015
Published in Issue Year 2015 Volume: 5 Issue: 3

Cite

APA Halaçoğlu, M. D., & Uğurlu, T. (2015). Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler. Clinical and Experimental Health Sciences, 5(3), 204-210. https://doi.org/10.5455/musbed.20150602014155
AMA Halaçoğlu MD, Uğurlu T. Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler. Clinical and Experimental Health Sciences. October 2015;5(3):204-210. doi:10.5455/musbed.20150602014155
Chicago Halaçoğlu, Mekin Doğa, and Timuçin Uğurlu. “Tabletler Ve Tablet basımına Etki Eden Kuvvetlerin Belirlenmesinde kullanılabilecek Bazı Yeni eşitlikler”. Clinical and Experimental Health Sciences 5, no. 3 (October 2015): 204-10. https://doi.org/10.5455/musbed.20150602014155.
EndNote Halaçoğlu MD, Uğurlu T (October 1, 2015) Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler. Clinical and Experimental Health Sciences 5 3 204–210.
IEEE M. D. Halaçoğlu and T. Uğurlu, “Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler”, Clinical and Experimental Health Sciences, vol. 5, no. 3, pp. 204–210, 2015, doi: 10.5455/musbed.20150602014155.
ISNAD Halaçoğlu, Mekin Doğa - Uğurlu, Timuçin. “Tabletler Ve Tablet basımına Etki Eden Kuvvetlerin Belirlenmesinde kullanılabilecek Bazı Yeni eşitlikler”. Clinical and Experimental Health Sciences 5/3 (October 2015), 204-210. https://doi.org/10.5455/musbed.20150602014155.
JAMA Halaçoğlu MD, Uğurlu T. Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler. Clinical and Experimental Health Sciences. 2015;5:204–210.
MLA Halaçoğlu, Mekin Doğa and Timuçin Uğurlu. “Tabletler Ve Tablet basımına Etki Eden Kuvvetlerin Belirlenmesinde kullanılabilecek Bazı Yeni eşitlikler”. Clinical and Experimental Health Sciences, vol. 5, no. 3, 2015, pp. 204-10, doi:10.5455/musbed.20150602014155.
Vancouver Halaçoğlu MD, Uğurlu T. Tabletler ve tablet basımına etki eden kuvvetlerin belirlenmesinde kullanılabilecek bazı yeni eşitlikler. Clinical and Experimental Health Sciences. 2015;5(3):204-10.

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